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A phytochemical study on the bark of Walsura pinnata has led to the isolation of a new oleanane triterpene acid, 3-oxo-olean-9(11),12-dien-28-oic acid (1), together with nine known compounds (2–10). Their structures were established on the basis of the detailed spectroscopic analysis, including one- and two-dimensional NMR, ESI-MS and HR-ESI-MS techniques. Compounds 2, 3, 5, 6 and 8 were isolated from W. pinnata for the first time. Compounds 3 and 4 showed in vitro growth inhibitory activity against two human cancer cell lines MCF-7 and SK-OV-3 with IC50 values within the range of 8.85 - 18.28 μg/mL. To the best of our knowledge, this is the first report on the cytotoxic activity of compound 3 towards both cancer cell lines.

Inhibition of acetylcholinesterase (AChE) enzyme is a known procedure to treat severe Alzheimer's disease through increasing the acetylcholine level in the brain and thus slowing down the progression of Alzheimer's symptoms. The approved medications are only considered as palliative and addressed some reported deficiencies. Therefore, the demand for safe and effective compounds is substantially increasing. A newly series of coumaryl 1,3-selenazoles derivatives was synthesized in four steps. Then, their antioxidant activities were evaluated using DPPH, ABTS cation radical scavenging assay and cupric reducing antioxidant capacities (CUPRAC). The anticholinesterase activities were evaluated using the Ellman method. Then, the docking studies were carried out to explain the possible correlation between in vitro anticholinesterase activity results and the ligand-receptor interactions. Ten new coumaryl 1,3-selenazoles (5a-5d series and 6a-6f series) derivatives were successfully synthesized. The DPPH radical scavenging assay showed that all tested compounds have IC50 value > 200 μM, for ABTS cation radical scavenging assay the IC50 value > 1000 μM and for CUPRAC assay the IC50 value > 200 μM. Compound 5c was found to be the most active compound against AChE and BChE in its series with IC50 value for AChE is 99.76 μM and IC50 for BChE is 140.28 μM while 6b exhibited the most potent inhibition in its series with IC50 value for AChE is 56.01 μM and IC50 for BChE is 121.34 μM. Besides, the docking studies showed that compound 5c and 6b formed π-π stacking interaction with aromatic residues at the active site of AChE and BChE, which is responsible for inhibiting the enzymes. This shows that the synthesized compounds contain skeletal structures that can interact and inhibit within the enzymes active site.

Aims: Acalypha indica (AI), Centella asiatica (CA), and Sesbania grandiflora (SG) are vegetables commonly used in traditional medicine in Asian countries to treat skin problems. In this study, we investigated their pharmacological activities relevant to wound healing and synergistic actions to provide an insight into a promising vegetable combination as a candidate treatment for wounds. Methodology and results: The stimulatory, antioxidant, and antibacterial activities of aqueous (A) and methanol (M) extracts of all the three vegetables were assessed alone and in combination in normal human dermal fibroblast (NHDF) cells in vitro. CA-A (89.52%) and the combination of AI-A+CA-A (90.76%) produced the highest percentage of wound closure. AI-A exhibited the highest total phenolic content (TPC) (82.94 mg GAE/g) and moderate reducing activity (61.63 mM Fe (II)/mg) when assessed by ferric reducing antioxidant power (FRAP) assay. Free radical scavenging activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid), and the combination of AI-A+CA-A exhibited scavenging activity at IC50 = 379.75 µg/mL and IC50 = 578.7 µg/mL, respectively. Pre-treatment of NHDF cells with CA-M at 100 µg/mL offered the highest protection against hydrogen peroxide. All single and combined vegetable extracts showed poor antibacterial properties against Gram negative and Gram positive bacterial species implicated in wound infection. Only AI-A+CA-A executed synergism in fibroblast migration when assessed via the combination index (CI). Furthermore, screening and identification of AI-A, CA-A, and CA-M via UHPLC (LC-MS/MS) system revealed that the major components responsible for all the tested bioactivities were phenolic groups such as simple polyphenols, flavonoids, polysaccharides, and triterpenes (asiaticoside and madecassosides). Conclusion, significance and impact of study: The vegetable extracts of A. indica, C. asiatica, and S. grandiflora exhibited good bioactivities independently. However, only AI-A+CA-A showed synergism in-combination to accelerate the migration of fibroblast and antioxidant activities. These findings demonstrate the potential formulation of combined vegetable extracts from the two species of A. indica and C. asiatica for optimum wound healing properties.

Aims:The oriental-based herbs Acalypha indica (AI), Centella asiatica (CA), and Sesbania grandiflora (SG) possess a broad range of undisclosed therapeutic activities which are edible and easily available throughout the year. To convert the herb extracts into a potential drug form, aqueous (A) and methanol (M) extracts of herbs were assessed alone and in combination for their antifungal-demelanising activity and nitric oxide (NO) immunomodulatory responses. A new bioactive synergistic and antagonistic assessments approach was made on these herbs to identify which extract combination qualifies as a natural drug candidate. Methodology and results: Via micro-dilution technique, methanol extract of A. indica (AI-M) showed the strongest antifungal activity against Aspergillus niger, with a minimum inhibitory concentration (MIC) of 50 mg/mL and a minimum fungicidal concentration (MFC) of 100 mg/mL. Sublethal (50 mg/mL) and subinhibitory (25 mg/mL) doses of AI-M produced the optimal black pigmentation reduction to demelanise A. niger. The combinations AI-M+CA-M, AI-M+SG-M, and CA-M+SG-M showed similar antifungal activities (MIC = 100 mg/mL). At 500 µg/mL, CA-A and the combination CA-A+SG-A successfully induced RAW264.7 cells to produce NO at 17.85 µM and 40.84 µM, respectively. The combination of herbs extract showed synergistic interaction towards stimulation of NO production. In contrast, they demonstrated antagonism towards antifungal-demelanising properties. Compound identification of AI-M, SG-M, and SG-A were performed using a UHPLC-QTrap-MS/MS system, which detected phenolic compounds from various groups (cinnamic acids, benzoic acids, and flavonoids). Conclusion, significance and impact of study: The combination of herb extracts showed better stimulation of NO production while the single herb extracts demonstrated good antifungal-demelanising activity. These findings help in the selection of herbs combination for potential natural drug discovery. A good combination of herbs demonstrated synergism to execute better bioactivities compared to individual herb extracts.